Abstract
A direct method using derivative spectrophotometry was developed for determining membrane-water molar partition coefficients (Kp) of the anticancer drugs tamoxifen (TAM) and 4-hydroxytamoxifen (OHTAM). This method explores a shift in the absorption spectra of the drugs when removed from the aqueous phase to a hydrophobic environment. Partition of TAM and OHTAM depends on membrane composition and on drug concentration, temperature and presence of cholesterol. Unlike OHTAM, partition of TAM in DMPC bilayers, liposomes of sarcoplasmic reticulum (SR) lipids and native membranes of SR and mitochondria decreases linearly with drug concentration. Additionally, the partition of these drugs is higher in SR native membranes than in liposomes of SR lipids. The partition also depends on membrane type, being higher in mitochondria than in SR membranes. Maximal partitionings in DMPC are observed at temperatures in the range of the main phase transition. Cholesterol strongly affects the incorporation of drugs and maximal inhibition was observed in DMPC bilayers.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: Biochemical and Biophysical Research Communications
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
